The cannabinoid CB1 receptor is expressed in pancreatic δ-cells

被引:42
|
作者
Tharp, William G. [1 ]
Lee, Yong-Ho [1 ]
Maple, Rhonda L. [1 ]
Pratley, Richard E. [1 ]
机构
[1] Univ Vermont, Coll Med, Diabet & Metab Translat Med Unit, Div Endocrinol Diabet & Metab,Dept Med, Burlington, VT 05405 USA
关键词
insulin; glucagon; somatostatin; pancreas; islet; obesity; diabetes; endocannabinoid; monoacylglycerol lipase; fatty acid amide hydrolase;
D O I
10.1016/j.bbrc.2008.05.077
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Antagonists of cannabinoid CB1 receptor (CB1, CNR1) promote weight loss and decrease hyperglycemia in patients with type 2 diabetes. While the endocannabinoid system may modulate islet hormone secretion, the cell-type expressing CB1 receptor in islets has not been fully resolved. In this study, we verified receptor gene expression in rodent islets and cell lines and examined the distribution of CB1 receptor in mouse, rat, and human islets by confocal immunofluorescence (IF) microscopy. IF demonstrated CBI receptor was present in beta-cell lines, but co-localized solely with somatostatin in the islet delta-cells of Zucker rats, C57BL/6 mice, and humans; no CB1 receptor expression was observed in alpha-, beta-, or pp-cells. Similarly, a rat somatostatinoma cell line, MSL-G2-Tu6, was found to express CB1 receptor. We also found monoacylglycerol lipase (MAGL) to be expressed in delta-cells and fatty acid amide hydrolase (FAAH) to be expressed in alpha-cells. The specific expression of CBI in delta-cells suggests that the ECS may play a role in modulating islet hormone secretion. As there are some differences between our findings and previous reports, further studies, including detailed physiological studies of the effects of the ECS on islet function, are warranted. (C) 2008 Elsevier Inc. All rights reserved.
引用
收藏
页码:595 / 600
页数:6
相关论文
共 50 条
  • [1] Similar in vitro pharmacology of human cannabinoid CB1 receptor variants expressed in CHO cells
    Xiao, Jing Chen
    Jewell, James P.
    Lin, Linus S.
    Hagmann, William K.
    Fong, Tung M.
    Shen, Chun-Pyn
    BRAIN RESEARCH, 2008, 1238 : 36 - 43
  • [2] CB1 cannabinoid receptor expression is regulated by glucose and feeding in rat pancreatic islets
    Vilches-Flores, Alonso
    Laura Delgado-Buenrostro, Norma
    Navarrete-Vazquez, Gabriel
    Villalobos-Molina, Rafael
    REGULATORY PEPTIDES, 2010, 163 (1-3) : 81 - 87
  • [3] Recent advances in CB1 cannabinoid receptor antagonists
    Lange, JHM
    Kruse, CG
    CURRENT OPINION IN DRUG DISCOVERY & DEVELOPMENT, 2004, 7 (04) : 498 - 506
  • [4] Pentacycle derivatives as cannabinoid CB1 receptor ligands
    Lee, Suk Ho
    Seo, Hee Jeong
    Kim, Min Ju
    Kang, Suk Youn
    Lee, Sung-Han
    Ahn, Kwangwoo
    Lee, MinWoo
    Han, Ho-Kyun
    Kim, Jeongmin
    Lee, Jinhwa
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (23) : 6632 - 6636
  • [5] Use of cannabinoid CB1 receptor antagonists for the treatment of metabolic disorders
    Scheen, Andre J.
    Paquot, Nicolas
    BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM, 2009, 23 (01) : 103 - 116
  • [6] Targeted proteomics of cannabinoid receptor CB1 and the CB1b isoform
    Ghosh, Soumita
    Gonzalez-Mariscal, Isabel
    Egan, Josephine M.
    Moaddel, Ruin
    JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2017, 144 : 154 - 158
  • [7] Differential Expression of CB1 Cannabinoid Receptor and Cannabinoid Receptor Interacting Protein 1a in Labor
    Kozakiewicz, Melissa L.
    Zhang, Jie
    Leone-Kabler, Sandra
    Yamaleyeva, Liliya M.
    McDonald, Anna G.
    Brost, Brian C.
    Howlett, Allyn C.
    CANNABIS AND CANNABINOID RESEARCH, 2022, 7 (03) : 279 - 288
  • [8] Binding Modes and Selectivity of Cannabinoid 1 (CB1) and Cannabinoid 2 (CB2) Receptor Ligands
    Yang, Jing-Fang
    Williams, Alexander H.
    Penthala, Narsimha R.
    Prather, Paul L.
    Crooks, Peter A.
    Zhan, Chang-Guo
    ACS CHEMICAL NEUROSCIENCE, 2020, 11 (20): : 3455 - 3463
  • [9] Cannabinoid CB1 receptor antagonists in therapeutic and structural perspectives
    Lange, Jos H. M.
    Kruse, Chris G.
    CHEMICAL RECORD, 2008, 8 (03) : 156 - 168
  • [10] Homology Modeling and Docking Studies of Cannabinoid Receptor CB1
    Tu Guogang
    Li Shaohua
    ACTA CHIMICA SINICA, 2011, 69 (08) : 1007 - 1010